| Literature DB >> 24314880 |
Nisha Mehta1, Maninder Kaur1, Manjinder Singh1, Sukhvir Chand1, Bhawna Vyas2, Pragati Silakari3, Malkeet Singh Bahia1, Om Silakari4.
Abstract
Purinergic receptors, also known as purinoceptors, are ligand gated membrane ion channels involved in many cellular functions. Among all identified purinergic receptors, P2X₇ subform is unique since it induces the caspase activity, cytokine secretion, and apoptosis. The distribution of P2X₇ receptors, and the need of high concentration of ATP required to activate this receptor exhibited its ability to function as 'danger' sensor associated with tissue inflammation and damage. Further, the modulation of other signalling pathways associated with P2X₇ has also been proposed to play an important role in the control of macrophage functions and inflammatory responses, especially towards lipopolysaccharides. Experimentally, researchers have also observed the decreased severity of inflammatory responses in P2X₇ receptor expressing gene (P2RX₇) knockout (KO) phenotypes. Therefore, newly developed potent antagonists of P2X₇ receptor would serve as novel therapeutic agents to combat various inflammatory conditions. In this review article, we tried to explore various aspects of P2X₇ receptors including therapeutic potential, and recent discoveries and developments of P2X₇ receptor antagonists.Entities:
Keywords: Caspase-1; Inflammasome; Interleukin-1β; P2X(7) receptor antagonists; Pro-inflammatory cytokines; Purinergic receptor; Toll like receptor (TLR)
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Year: 2013 PMID: 24314880 DOI: 10.1016/j.bmc.2013.10.054
Source DB: PubMed Journal: Bioorg Med Chem ISSN: 0968-0896 Impact factor: 3.641